Journal of medicinal chemistry

Convenient synthesis of 10-deazaaminopterin via a pteridine ylide

JR Piper, JA Montgomery

文献索引：Piper, James R.; Montgomery, John A. Journal of Medicinal Chemistry, 1980 , vol. 23, # 3 p. 320 - 321

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被引用次数: 13

摘要

10-Deazaaminopterin, a potential antitumor agent now undergoing clinical trials, has been synthesized by a new approach involving the Wittig reaction. The ylide obtained by reaction of 6-(bromomethyl)-2, 4-pteridinediamine with triphenylphosphine in Me2NAc, followed by treatment with NaOMe, underwent smooth reaction with diethyl N-(4-formylbenzoyl)-~- glutamate to give the vinyl precursor of the subject compound. Catalytic hydrogenation (Pt ...